A heme-activatable probe and its application in the high-throughput screening of Plasmodium falciparum ring-stage inhibitors  

作　　者：Sheng Liu Chunyan Wei Tian Liu Shuang-Gang Ma Chen Chen Hao Lin Lianhui Zhang Heng Wang Chong-Jing Zhang Shi-Shan Yu 

机构地区：[1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines and Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China [2]Department of Microbiology and Parasitology,Institute of Basic Medical Sciences Chinese Academy of Medical Sciences,School of Basic Medicine Peking Union Medical College,5#Dong Dan San Tiao,Beijing 100005,China

出　　处：《Signal Transduction and Targeted Therapy》2022年第6期1882-1884,共3页信号转导与靶向治疗（英文）

基　　金：supported by the following funding:The Natural Science Foundation of China(No.21732008);CAMS Innovation Fund for Medical Sciences(CIFMS)(2016-I2M-3-010,2017-I2M-4-005,2016-I2M-1-019).

摘　　要：Dear Editor,The resistance of Plasmodium falciparum to artemisinin derivatives(ARTs)in Asian,African and South American countries is a pressing global concern.Heme is an important biomarker of malaria parasites and is closely related to the mode of action of ARTs,but no heme-activatable fluorescent probe has been developed to study the biology of heme in malaria parasites in a light-up manner.Here,we rationally developed probes from the unique reaction between heme and Yingzhaosu A(YZSA),then we unprecedentedly applied the probe to identify ring-stage inhibitors of P.falciparum.

关 键 词：FALCIPARUM HEME PLASMODIUM 

分 类 号：R53[医药卫生—内科学]